PMID- 23162904 OWN - NLM STAT- MEDLINE DCOM- 20130926 LR - 20121119 IS - 0513-4870 (Print) IS - 0513-4870 (Linking) VI - 47 IP - 8 DP - 2012 Aug TI - [In vitro and in vivo evaluation of total flavones of Hippophae rhamnoides self-microemulsifying drug delivery system]. PG - 1055-62 AB - The goal of the study is to evaluate the self-microemulsifying drug delivery system (SMEDDS) which enhances the oral bioavailability of the poorly water-soluble drug, total flavones of Hippophae rhamnoides (TFH). It is orally administered for the protection of human cardiovascular system. Self-microemulsifying time, particle size, polydispersity index (PDI), morphological characterization, in vitro dispersity, stability, in situ intestinal absorption and relative bioavailability were investigated in detail. The TFH-SMEDDS rapidly formed fine oil-in-water microemulsions with 0.1 mol x L(-1) hydrochloride solution, with average size of which was less than 40 nm, PDI was below 0.2, and the particles of which were observed round-shaped under transmission electron microscope. Almost 90% of TFH (expressed with quercetin) was released from SMEDDS within 20 min, which was remarkably higher than that from common capsules. The stability test showed the TFH-SMEDDS maintained stable in 6 months under accelerated condition. In situ absorption study demonstrated the absorption rate constant of TFH-SMEDDS (expressed with quercetin) was significantly higher than that of TFH in ethanolic solution (P < 0.05). The absorption of TFH from SMEDDS showed a 4.18-fold increase in relative bioavailability (expressed with quercetin) compared with that of the suspension. The results suggest that SMEDDS is a promising drug delivery system to increase the oral bioavailability of TFH. FAU - Li, Gui-ling AU - Li GL AD - Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. FAU - Fan, Ya-ting AU - Fan YT FAU - Zhang, Yan-hui AU - Zhang YH FAU - Li, Yan-fang AU - Li YF FAU - Li, Xin-ru AU - Li XR FAU - Liu, Yan AU - Liu Y FAU - Li, Mei AU - Li M LA - chi PT - English Abstract PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - China TA - Yao Xue Xue Bao JT - Yao xue xue bao = Acta pharmaceutica Sinica JID - 21710340R RN - 0 (Drug Carriers) RN - 0 (Emulsions) RN - 0 (Flavones) SB - IM MH - Administration, Oral MH - Animals MH - Biological Availability MH - Drug Carriers MH - *Drug Delivery Systems MH - Emulsions MH - Flavones/administration & dosage/isolation & purification/*pharmacokinetics MH - Fruit/chemistry MH - Hippophae/*chemistry MH - *Intestinal Absorption MH - Male MH - Particle Size MH - Plant Leaves/chemistry MH - Plants, Medicinal/chemistry MH - Random Allocation MH - Rats MH - Rats, Sprague-Dawley EDAT- 2012/11/20 06:00 MHDA- 2013/09/27 06:00 CRDT- 2012/11/20 06:00 PHST- 2012/11/20 06:00 [entrez] PHST- 2012/11/20 06:00 [pubmed] PHST- 2013/09/27 06:00 [medline] PST - ppublish SO - Yao Xue Xue Bao. 2012 Aug;47(8):1055-62.